MI-2 (Menin-MLL Inhibitor)

SKU: orb1226629

Description

MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.

Key Properties

• CAS Number: 1271738-62-5
• MW: 375.55
• Purity: >98% (HPLC)
• Formula: C₁₈H₂₅N₅S₂
• SMILES: CCCC1=CC2=C(N3CCN(C4=NCC(C)(C)S4)CC3)N=CN=C2S1
• Target: HMTase
• Solubility: Ethanol: 75 mg/mL (199.7 mM); DMSO: 75 mg/mL warmed (199.7 mM)

Bioactivity

• In Vitro:
  Menin-MLL inhibitor MI-2 very effectively blocks proliferation of MLL-AF9 and MLL-ENL transduced BMC, with GI50 values of about 5 μM. Assessment of diverse hydrophobic groups at R1 led to the development of several compounds with IC50 values in the nanomolar range, including MI-2 (IC50 = 446±28 nM) and MI-3 (IC50 = 648±25 nM). The dissociation constants measured for the menin-MLL inhibitors are at the nanomolar level, Kd=158 nM for MI-2. MI-2 can access the protein target and very effectively inhibit the menin-MLL-AF9 interaction in human cells. Furthermore, MI-2 shows only a small effect on the cell growth of E2A-HLF transduced BMC (GI50>50 μM), which may be due to inhibition of the menin interaction with wild-type MLL. Treatment with MI-2 results in GI50 values below 10 μM in MV4; 11 (harboring MLL-AF4; GI50 = 9.5 μM), KOPN-8 (MLL-ENL; GI50 = 7.2 μM) and ML-2 (MLL-AF6; GI50 = 8.7 μM), and in MonoMac6 (MLL-AF9; GI50 = 18 μM).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Menin-MLL Inhibitor

Quick Database Links

Gene Symbol

HMTase